One of the basic phenomena of life is that living creatures take food from their environment. Considering that for the living creatures both overfeeding and underfeeding are dangerous, simultaneously with the rise of the food intake also a system for controlling the food intake has been developed. Together with the development of life also this food intake control system became more and more developed and today it operates as a very complicated system "having several regulating circles". (A summary of some presumed and proved regulating mechanisms is given in The Lancet of Feb. 19, 1983 on pages 398 to 401.) One of these regulating mechanisms is based on the so called opioid endogenic peptides. This is supported by the observation that if a special opiate antagonist, naloxone [(5.alpha.)- 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-morphinane-6-one] is administered to animals it is absorbed by the opiate receptors and thereby the food intake, the appetite and also the fluid intake of the animal is hindered. The observation that by the administration of endogenic (and exogenic) opiates the appetite of animals and humans can be increased shows that these compounds exert an influence on the nutrition (Am. J. Clin. Nutr., 35, 757-761, 1982 and Appetite, 2, 193-208, 1981).
While in the case of non-domesticated animals the regulating mechanisms function more or less properly and ensure the appropriate food intake of the animals, in the case of humans complications from overeating are a common problem.
This can be readily understood as in the case of humans, food intake is caused not only by the sensation of hunger and, often the degree of the food intake does not merely follow the demands of the organism, and the demands are often many time surpassed. It is true that by careful food intake obesity can be avoided but in many instances the decision in itself is not sufficient for changing the alimentary habits, therefore for carrying out the decision a medical support is necessary as well.
The best known slimming agents are desopimone (4-chloro-.alpha.,.alpha.-dimethyl-phenethylamine), gracidine (3-methyl-2-phenyl-morpholine) and teronac [5-(p-chloro-phenyl)-2,5-dihydro-3H-imidazo[2,1-a]isoindole-5-ol].
Unfortunately the known slimming agents have several contraindications and side effects, so in the case of a great number of the patients requiring treatment these agents cannot be used.
The side effects of desopimone are the dilatation of the pupil, increase of the inner pressure of the eyes, vomiting, diarrhoea, abdominal pains, difficulty at the beginning of urination, headache, allergic exanthema, vertigo; and insomnia and nervosity as well as somnolence and sedative effect all appearing in about equal proportions.
Gracidine only with increased care can be administered in the case of obesity associated with heart diseases, cardiovascular troubles and hypertension. At the intake of gracidine and when it is administered continuously during the treatment the driving of vehicles, working above ground and on dangerous machines are prohibited. During its use and influence, respectively, also the consumption of alcoholic drinks is prohibited. According to new information the compositions containing gracidine are forbidden.
Teronac may cause mouth dryness, headache, nervosity, nausea, constipation, impairment of sleep, dizziness, tachycardia, reversible trouble of sexual functions, sweating, eczema, dilatation of the pupil, allergy. Also in case of glaucoma, heart-rhythm troubles, serious cardiac failure, renal insufficiencies, liver troubles, hypertension, cerebral disturbances, psychiatric diseases, gastric and intestinal ulcers, the drug is contraindicated.
On the basis of the aforesaid an appetite reducing composition is needed which does not show the side effects of the known compositions and which can be widely used without side effects.
As the active ingredient of a composition like this primarily those substances can be taken into consideration which exert their influence on the field of the central nervous system. Substances of this type are also the opiate antagonists mentioned above.
It is known that in obese people the food intake is reduced by naloxone (J. Clin. Endocrin, Metab., 55, 196-198, 1982). It has similar activity in Prader-Willi syndrome (The Lancet, 1980, 876-877), traumatic hypothalamic hyperphagia (Am. J. Clin. Nutr., 35, 757-761, 1982) and also in the case of healthy patients rendered hungry by 2-desoxy-glucose infusion.
The use of naloxone as active ingredient in appetite reducing compositions is unavoidably hindered by the fact that when administered per os it should be given in extremely high doses. But in the case of a widely used appetite reducing composition only the peroral administration can come into consideration.
The object of the present invention is to provide an appetite reducing composition which can be widely used without side effects and contraindications.